title: Tricyclic heteroaromatic systems. 1,2,4-triazolo[4,3-a]quinoxalines and 1,2,4-Triazino[4,3-a]quinoxalines: synthesis and central benzodiazepine receptor activity.
abstract: Some 1,2,4-triazolo[4,3-a]quinoxalines 1-10, and 1,2,4-triazino[4,3-a]quinoxalines 11-12 were prepared and biologically evaluated for their binding at the benzodiazepine receptor (BZR) in rat cortical membranes. The BZR affinity of 1-10 demonstrates that the presence of a proton acceptor at position-1 is important for the potency of a BZR ligand. On the other hand, the BZR inactivity of the 1,2,5-trione derivatives 11-12 shows that the right collocation of the essential L2 lipophilic substituent is of paramount importance for receptor-ligand interaction.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.
authors.forename: V
authors.initials: V
authors.lastname: Colotta
authors.forename: D
authors.initials: D
authors.lastname: Catarzi
authors.forename: F
authors.initials: F
authors.lastname: Varano
authors.forename: L
authors.initials: L
authors.lastname: Cecchi
authors.forename: G
authors.initials: G
authors.lastname: Filacchioni
authors.forename: A
authors.initials: A
authors.lastname: Galli
authors.forename: C
authors.initials: C
authors.lastname: Costagli
mesh_terms: D000818:Animals; D002540:Cerebral Cortex / Q000378:metabolism*; D008297:Male; D011810:Quinoxalines / Q000138:chemical synthesis / Q000378:metabolism*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011963:Receptors, GABA-A / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000378:metabolism*
chemical_list: D011810:Quinoxalines; D011963:Receptors, GABA-A; D014230:Triazoles